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Ursolic acid loaded tri-block copolymer nanoparticles based on triphenylphosphine for mitochondria-targeted cancer therapy.
Biomedical Materials 2024 Februrary 30
A novel biodegradable amphiphilic triblock copolymer, PAEEP-PEG-PLLA(polyphosphate, polyethylene glycol, and polylactic acid), was synthesized by twice ring-opening polymerization and triphenylphosphine (TPP) was grafted onto the block copolymer to synthesize a carrier material (TPP-PAEEP-PEG-PLLA), which was identified by 1H-NMR spectroscopy. The TPP-PAEEP-PEG-PLLA nanoparticles encapsulated with ursolic acid were prepared by the emulsion-solvent evaporation method and characterized by dynamic light scattering. The mitochondrial targeting ability of fluorescently labeled nanoparticles was evaluated by laser confocal microscopy. The average particle size and surface charge of the ursolic acid-loaded nanoparticle solution were 180.07±1.67 nm and +15.57±1.33 mV, respectively. The biocompatibility of nanoparticles was briefly evaluated by erythrocyte hemolysis assay. In vitro cell proliferation assay and scratch migration assay were performed to compare the difference in anti-tumor effect between ursolic acid and ursolic acid nanoparticles. The results showed that triphenylphosphine-modified triblock copolymers had good mitochondrial targeting and improved the low bioavailability of ursolic acid, and ursolic acid nanoparticles exhibited more pronounced anti-tumor capabilities. In summary, the results suggested that our ursolic acid nanoparticles were a promising drug-targeted delivery system for the treatment of tumors.
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